695172-02-2Relevant articles and documents
The first potent diphenyl phosphonate KLK4 inhibitors with unexpected binding kinetics
Van Soom, Jeroen,Cuzzucoli Crucitti, Giuliana,Gladysz, Rafaela,Van Der Veken, Pieter,Di Santo, Roberto,Stuyver, Ingmar,Buck, Victoria,Lambeir, Anne-Marie,Magdolen, Viktor,Joossens, Jurgen,Augustyns, Koen
, p. 1954 - 1958 (2015/11/17)
KLK4 is a serine protease from the kallikrein family that is involved in cancer progression. The diphenyl phosphonate warhead is intended to bind irreversibly with serine proteases, but unexpectedly, very potent KLK4 diphenyl phosphonate inhibitors were d
Novel Urokinase Inhibitors
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Page/Page column 28; 30, (2009/01/24)
The present invention relates to novel compounds with inhibitory activity towards urokinase plasminogen activator (uPA); to methods for preparation of said uPA inhibitor compounds; to pharmaceutical compositions comprising said uPA inhibitor compounds; to
A p-[18F]fluoroethoxyphenyl bicyclic nucleoside analogue as a potential positron emission tomography imaging agent for varicella-zoster virus thymidine kinase gene expression
Chitneni, Satish K.,Deroose, Christophe M.,Balzarini, Jan,Gijsbers, Rik,Celen, Sofie,Debyser, Zeger,Mortelmans, Luc,Verbruggen, Alfons M.,Bormans, Guy M.
, p. 6627 - 6637 (2008/09/17)
We recently reported a new positron emission tomography (PET) reporter gene, namely, varicella-zoster virus thymidine kinase (VZV-tk) in combination, with carbon-11 or fluorine-18 labeled m-alkoxyphenyl bicyclic nucleoside analogues (BCNAs) as PET reporte
Small, potent, and selective diaryl phosphonate inhibitors for urokinase-type plasminogen activator with in vivo antimetastatic properties
Joossens, Jurgen,Ali, Omar M.,El-Sayed, Ibrahim,Surpateanu, Georgiana,Der Van Veken, Pieter,Lambeir, Anne-Marie,Setyono-Han, Buddy,Foekens, John A.,Schneider, Anneliese,Schmalix, Wolfgang,Haemers, Achtel,Augustyns, Koen
, p. 6638 - 6646 (2008/09/17)
A set of small nonpeptidic diaryl phosphonate inhibitors was prepared. Some of these inhibitors show potent and highly selective irreversible uPA inhibition. The biochemical and modeling data prove that the combination of a benzylguanidine moiety with a d
NOVEL UROKINASE INHIBITORS
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Page/Page column 81-83; 85-86, (2010/11/27)
The present invention relates to novel compounds with inhibitory activity towards urokinase plasminogen activator (uPA); to methods for preparation of said uPA inhibitor compounds; to pharmaceutical compositions comprising said uPA inhibitor compounds; to
Diphenyl phosphonate inhibitors for the urokinase-type plasminogen activator: Optimization of the P4 position
Joossens, Jurgen,Van Der Veken, Pieter,Surpateanu, Georgiana,Lambeir, Anne-Marie,El-Sayed, Ibrahim,Ali, Omar M.,Augustyns, Koen,Haemers, Achiel
, p. 5785 - 5793 (2007/10/03)
This paper describes the structure-activity relationship in a series of tripeptidyl diphenyl phosphonate irreversible urokinase plasminogen activator (uPA) inhibitors, originally derived from an arginyltripeptide. uPA is considered an interesting target i
Development of Irreversible Diphenyl Phosphonate Inhibitors for Urokinase Plasminogen Activator
Joossens,Van Der Veken,Lambeir,Augustyns,Haemers
, p. 2411 - 2413 (2007/10/03)
In this letter we report the synthesis and biochemical evaluation of selective, irreversible diphenyl phosphonate inhibitors for urokinase plasminogen activator (uPA). A diphenyl phosphonate group was introduced on the substratelike peptide Z-D-Ser-Ala-Arg, and modification of the guanidine side chain was investigated. A guanylated benzyl group appeared the most promising side chain modification. A kapp value in the 103 M -1 s-1 range for uPA was obtained, together with a selectivity index higher than 240 toward other trypsin-like proteases such as tPA, thrombin, plasmin, and FXa.
